MRT-9643 | CDK2 degrader | Probechem Biochemicals

Chemical Structure : MRT-9643

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MRT-9643 (MRT9643)

货号: PC-24595Not For Human Use, Lab Use Only.

MRT-9643 (MRT9643) is a potent, selective and orally active CDK2-directed molecular glue degrader, induces CDK2-dependent cancer cell growth inhibition.

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生物&药学活性

MRT-9643 (MRT9643) is a potent, selective and orally active CDK2-directed molecular glue degrader, induces CDK2-dependent cancer cell growth inhibition.
MRT-9643 engages CDK2 through a novel binding mode that does not utilize the catalytic site typically engaged by catalytic-site inhibitors, enabling superior selectivity over conserved CDKs and other kinases.
The combination of MRT-9643 and Ribociclib (CDK4/6 inhibitor) delayed resistance to CDK4/6 inhibition both in vitro and in vivo.
MRT-9643 drove deep tumor regression in combination with a CDK4/6 inhibitor or triple combination with a CDK4/6 inhibitor and endocrine therapy (fulvestrant), resulting in enhanced downstream pathway suppression as compared to a CDK4/6 inhibitor alone in preclinical models of HR-positive/HER2-negative breast cancer.

物理化学性质&存储条件

分子量	511.45
分子式	C23H22F5N5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(2,6-difluoro-4-((2R,3S)-2-methyl-3-((5-(3-(trifluoromethyl)bicyclo[1.1.1]pentan-1-yl)-1,3,4-oxadiazol-2-yl)amino)azetidin-1-yl)phenyl)piperidine-2,6-dione

参考文献

1. Patent WO2024092039 A1.

MRT-9643 (MRT9643)

生物&药学活性

物理化学性质&存储条件

参考文献

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询单

MRT-9643 (MRT9643)

生物&药学活性

物理化学性质&存储条件

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